Capacity of cholesteryl hemisuccinate in ion pair/phospholipid complex to improve drug-loading, stability and antibacterial activity of clarithromycin intravenous lipid microsphere

2018 ◽  
Vol 172 ◽  
pp. 262-271 ◽  
Author(s):  
Lifeng Luo ◽  
Qiuyue Chen ◽  
Haoyu Gong ◽  
Lu Liu ◽  
Lingli Zhou ◽  
...  
Author(s):  
Rassoul Dinarvand ◽  
TS Jafarzadeh Kashi ◽  
Eskandarion ◽  
Esfandyari-Manesh ◽  
Samadi ◽  
...  

2021 ◽  
Vol 8 ◽  
Author(s):  
Qi Liu ◽  
Wen-Chong Ouyang ◽  
Xiu-Hong Zhou ◽  
Tao Jin ◽  
Zheng-Wei Wu

In this study, nanofibers with different ratios of poly(vinyl alcohol) and chitosan incorporated with moxifloxacin hydrochloride (MH/PVA/CS) were fabricated through the blending electrospinning, and the morphological features were tested using scanning electron microscopy (SEM). Further characterization of the new nanofiber was accomplished by Thermogravimetric analysis (TG), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FTIR). Antibacterial activity of the MH-loaded nanofibers at different drug loading were tested and compared with the blank group. Experimental results show that the MH/PVA/CS nanofibers exhibited the good antibacterial properties against Staphylococcus aureus and Pseudomonas aeruginosa due to the MH incorporation. Compared with blank nanofibers, MH/PVA/CS nanofibers have significantly better antibacterial properties, and different proportions of PVA and CS have a certain effect on the antibacterial activity of nanofibers. The conclusions in this paper show that MH/PVA/CS composite nanofibers may have great potential in antibacterial materials.


2021 ◽  
Vol 9 ◽  
Author(s):  
Dandan Hong ◽  
Jingjing Wu ◽  
Xuemin Xiao ◽  
Xueyang Li ◽  
Dong Xu ◽  
...  

Antimicrobial peptides (AMPs) have great potential for clinical treatment of bacterial infection due to the broad-spectrum and highly effective antibacterial activity. However, the easy degradation and inactivation in vivo has been a major obstacle for their application and an effective delivery system is demanding. The surface physicochemical properties of the carrier, including surface potential, surface polarity, pore structure and morphology, have exerted great effects on the adsorption and release behavior of AMPs. This study investigated the influence of micro/nano carriers with different hierarchical structures on the loading, release and biological behavior of AMPs. Three types of AMPs-loaded hydroxyapatite microspheres (HA/AMPs MSs) with different hierarchical structures (needle-like, rod-like, and flake-like) were developed, which was investigated by the surface morphology, chemical composition and surface potential in detail. The different hierarchical structures of hydroxyapatite microspheres (HA MSs) had noticeable impact on the loading and release behavior of AMPs, and the flake-like HA MSs with hierarchical structure showed the highest loading efficiency and long-lasting release over 9 days. Meanwhile, the stability of AMPs released from HA MSs was effectively maintained. Moreover, the antibacterial test indicated that the flake-like HA/AMPs MSs showed more sustained antibacterial properties among three composites. In view of the excellent biocompatibility and osteogenic property, high loading efficiency and the long-term release properties of HA MSs with hierarchical structure, the HA/AMPs MSs have a great potential in bone tissue engineering.


2019 ◽  
Vol 25 (34) ◽  
pp. 3692-3701 ◽  
Author(s):  
Hanif Ullah ◽  
Munair Badshah ◽  
Alexandra Correia ◽  
Fazli Wahid ◽  
Hélder A. Santos ◽  
...  

Background: Bacterial cellulose (BC) has recently attained greater interest in various research fields, including drug delivery for biomedical applications. BC has been studied in the field of drug delivery, such as tablet coating, controlled release systems and prodrug design. Objective: In the current work, we tested the feasibility of BC as a drug carrier in microparticulate form for potential pharmaceutical and biomedical applications. Method : For this purpose, drug-loaded BC microparticles were prepared by simple grinding and injection moulding method through regeneration. Model drugs, i.e., cloxacillin (CLX) and cefuroxime (CEF) sodium salts were loaded in these microparticles to assess their drug loading and release properties. The prepared microparticles were evaluated in terms of particle shapes, drug loading efficiency, physical state of the loaded drug, drug release behaviour and antibacterial properties. Results: The BC microparticles were converted to partially amorphous state after regeneration. Moreover, the loaded drug was transformed into the amorphous state. The results of scanning electron microscopy (SEM) showed that microparticles had almost spherical shape with a size of ca. 350-400 μm. The microparticles treated with higher drug concentration (3%) exhibited higher drug loading. Keeping drug concertation constant, i.e., 1%, the regenerated BC (RBC) microparticles showed higher drug loading (i.e., 37.57±0.22% for CEF and 33.36±3.03% for CLX) as compared to as-synthesized BC (ABC) microparticles (i.e., 9.46±1.30% for CEF and 9.84±1.26% for CLX). All formulations showed immediate drug release, wherein more than 85% drug was released in the initial 30 min. Moreover, such microparticles exhibited good antibacterial activity with larger zones of inhibition for drug loaded RBC microparticles as compared to corresponding ABC microparticles. Conclusion : Drug loaded BC microparticles with immediate release behaviour and antibacterial activity were fabricated. Such functionalized microparticles may find potential biomedical and pharmaceutical applications.


Author(s):  
Dr. Muhammad Abuzar Raza Naqvi ◽  

The main aims of this manuscript are to: i) investigate the high drug loading of cefazolin and its characterization, ii), demonstrate the bioactivity of the cefazolin particles in vitro on Staphylococcus aureus. From our results, it is observed that the cefazolin loading into MCM-41 particles is 34 wt %. Furthermore, particles showed the burst release of cefazolin at pH 6.8. At higher concentration, MCM-41 particles are comparatively more cytotoxic as compared to lower concentration. Finally, cefazolin loaded particles showed higher in vitro antibacterial activity against Staphylococcus aureus as compared to cefazolin only.


2018 ◽  
Vol 89 (17) ◽  
pp. 3506-3518 ◽  
Author(s):  
Jin Jeong ◽  
Seungsin Lee

Coptidis Rhizoma is a medicinal plant that is well known for its high antibacterial activity against various pathogens and its anti-inflammatory, antioxidant, and hemostatic effects. Here, nanofibrous membranes containing 10, 20, and 30 wt% of Coptidis Rhizoma extracts were fabricated by electrospinning using poly(vinyl alcohol) as the drug carrier and thermally treated to increase their aqueous stability. The antibacterial properties and release characteristics of Coptidis Rhizoma nanofibrous membranes were investigated. Coptidis Rhizoma-loaded nanocomposite fibers exhibited a high drug-loading efficiency ranging from 92% to 97%. The release profile from the nanofibrous membranes of Coptidis Rhizoma showed an initial fast release followed by a gradual release for 48 h. High antibacterial activity of the Coptidis Rhizoma-loaded nanofibrous membranes was exhibited against both Staphylococcus aureus and Staphylococcus epidermidis. These results demonstrate that poly(vinyl alcohol) nanofibrous membranes containing Coptidis Rhizoma extracts have considerable potential to be effective antimicrobial wound dressings based on natural substances.


2020 ◽  
Vol 25 (6) ◽  
pp. 598-607
Author(s):  
Mustafa E. Omer ◽  
Majed Halwani ◽  
Rayan M. Alenazi ◽  
Omar Alharbi ◽  
Shokran Aljihani ◽  
...  

Ciprofloxacin (CIP), a widely used antibiotic, is a poor biopharmaceutical resulting in low bioavailability. We optimized a CIP polymer–lipid hybrid nanoparticle (CIP-PLN) delivery system to enhance its biopharmaceutical attributes and the overall therapeutic performance. CIP-PLN formulations were prepared by a direct emulsification–solvent–evaporation method. Varying the type and ratio of lipid was tried to optimize a CIP-PLN formulation. All the prepared formulations were evaluated for their particle size, polydispersity index, zeta potential, physical stability, and drug entrapment efficiency. The drug in vitro release profile was also studied. Antibacterial activities were tested by the agar diffusion method for all CIP-PLN formulations against an Escherichia coli clinical bacterial isolate (EC04). CIP-PLN formulations showed average sizes in the range of 133.9 ± 1.7 nm to 217.1 ± 0.8 nm, exhibiting high size uniformity as indicated by polydispersity indices lower than 0.25. The entrapment efficiency was close to 80% for all formulations. The differential scanning calorimetry (DSC) thermograms indicated the existence of CIP in the amorphous state in all PLN formulations. Fourier transform infrared spectra indicated deep incorporation of molecular CIP within the polymer matrix. The release profile of CIP from PLN formulas showed a uniform prolonged drug profile, extended for a week from most formulations with a zero-order kinetics. The antibacterial activity of CIP-PLN formulations showed significantly higher antibacterial activity only with F4 containing lecithin as the lipid component. In conclusion, we successfully optimized a CIP-PLN formulation with a low nanoparticle size in a close range, high percentage of entrapment efficiency and drug loading, uniform prolonged release rate, and higher antibacterial activity against the EC04 clinical isolate.


2014 ◽  
Vol 26 (03) ◽  
pp. 1450041 ◽  
Author(s):  
J. Suwanprateeb ◽  
F. Thammarakcharoen ◽  
P. Phanphiriya ◽  
W. Chokevivat ◽  
W. Suvannapruk ◽  
...  

In this study, preparation and characterization of antibiotic-impregnated microporous nano-hydroxyapatite (HA) aiming to function as both antibiotic carrier and bone graft for osteomyelitis treatment were carried out. Microporous nano-hydroxyapatite was prepared by low temperature phosphorization of three-dimensional printed calcium sulfate sample and was impregnated by three types of antibiotics including vancomycin, fosfomycin and gentamicin. Materials properties and antibacterial performance including phase composition, microstructure, degradability, total drug loading, antibacterial activity and shelf life were investigated and reported. Microporous nano-hydroxyapatite having porosity and mean pore size of 63.92% and 0.15 microns was prepared and showed greater resorbability than typical high-temperature sintering samples. Sustained release of antibiotic from the impregnated samples for longer than 29 days was observed, but the difference in the efficiency was related to the difference in the molecular weight, mechanism of action, spectrum of activity of each antibiotic. No deterioration in the antibacterial activity of the prepared antibiotic-impregnated hydroxyapatite was observed after storing for up to 12 months. No cytotoxic potential by MTT assay at all extraction periods was observed for vancomycin-impregnated hydroxyapatite. Gentamicin and fosfomycin impregnated hydroxyapatites showed cytotoxic potential only on day 1 extraction, but no cytotoxic potential was observed on day 2 extraction onward. This could be related to the concentration and characteristics of each released antibiotics.


Sign in / Sign up

Export Citation Format

Share Document